Abstract
Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.
Keywords: ABCB1 inhibitor, structure-activity relationships, ABCB1 substrate properties
Medicinal Chemistry
Title:Novel Structurally Varied N-Alkyl 1,4-Dihydropyridines as ABCB1 Inhibitors: Structure-Activity Relationships, Biological Activity and First Bioanalytical Evaluation
Volume: 9 Issue: 4
Author(s): Andreas Hilgeroth, Christiane Baumert, Claudius Coburger, Marianne Seifert, Soren Krawczyk, Cornelius Hempel, Felix Neubauer, Martin Krug, Josef Molnar and Hermann Lage
Affiliation:
Keywords: ABCB1 inhibitor, structure-activity relationships, ABCB1 substrate properties
Abstract: Series of structurally varied N-alkyl 1,4-dihydropyridines and novel benzo-annelated derivatives as 1,4- dihydroquinolines have been characterized as ABCB1 inhibitors. Structure-activity relationships (SARs) are discussed. Cytotoxic activities of selected compounds have been determined. A first bioanalysis of ABCB1 substrate properties has been carried out in a cell-based model. Compounds with highest ABCB1 inhibiting activities were no substrates of ABCB1 and not transported by the efflux pump, thus profiling the new ABCB1 inhibitors.
Export Options
About this article
Cite this article as:
Hilgeroth Andreas, Baumert Christiane, Coburger Claudius, Seifert Marianne, Krawczyk Soren, Hempel Cornelius, Neubauer Felix, Krug Martin, Molnar Josef and Lage Hermann, Novel Structurally Varied N-Alkyl 1,4-Dihydropyridines as ABCB1 Inhibitors: Structure-Activity Relationships, Biological Activity and First Bioanalytical Evaluation, Medicinal Chemistry 2013; 9 (4) . https://dx.doi.org/10.2174/1573406411309040002
DOI https://dx.doi.org/10.2174/1573406411309040002 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Targeting Transcription Factor Binding to DNA by Competing with DNA Binders as an Approach for Controlling Gene Expression
Current Topics in Medicinal Chemistry DLEU1: A Functional Long Noncoding RNA in Tumorigenesis
Current Pharmaceutical Design Meet Our Associate Editor
Current Molecular Medicine The Unbiased Search of Biomarkers in Neurodegenerative Diseases
Current Pharmaceutical Biotechnology Targeting Signaling Pathways in Multiple Myeloma
Current Pharmaceutical Biotechnology Defensin Participation in Innate and Adaptive Immunity
Current Pharmaceutical Design Regulation of Hypoxia-inducible Factor-1α and Vascular Endothelial Growth Factor Signaling by Plant Flavonoids
Mini-Reviews in Medicinal Chemistry Study of Cancer Cell Lines with Fourier Transform Infrared (FTIR)/ Vibrational Absorption (VA) Spectroscopy
Current Physical Chemistry High Throughput Microfluidic Electrical Impedance Flow Cytometry for Assay of Micro Particles
Micro and Nanosystems Anticancer Activity and DNA Binding of 4-Alkylenediamines Modified Naphthalimide Derivatives
Letters in Drug Design & Discovery The TGF-β Signaling Pathway as a Pharmacological Target in a Hepatocellular Carcinoma
Current Pharmaceutical Design Growth Factors as Therapeutics for Diabetic Neuropathy
Current Drug Targets Leptin, Estrogens and Cancer
Mini-Reviews in Medicinal Chemistry Nongenomic Actions of Retinoids: Role of Nur77 and RXR in the Regulation of Apoptosis and Inflammation
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cancer and Aids: New Trends in Drug Design and Chemotherapy
Current Computer-Aided Drug Design Gene Therapy Using IL-12 Family Members in Infection, Auto-Immunity, and Cancer
Current Gene Therapy Chemical Advances in Therapeutic Application of Exosomes and Liposomes
Current Medicinal Chemistry The p53 Pathway Encounters the MicroRNA World
Current Genomics Antisense Oligonucleotides in the Treatment of Cerebral Gliomas. Review of Concerning Patents
Recent Patents on CNS Drug Discovery (Discontinued) Drug Targets to Pro-Angiogenetic Factors with Special Reference to Primary Peritoneal Mesothelioma
Endocrine, Metabolic & Immune Disorders - Drug Targets